Tazemetostat hydrochloride

Tazemetostat (EPZ-6438) hydrochloride is a potent, selective and orally active EZH2 inhibitor with IC50 values of 11 and 16 nM for EZH2 peptide and nucleosome, respectively. Tazemetostat hydrochloride can be used for cancer research[1].

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Histone Methyltransferase

Tazemetostat (EPZ-6438; 0.49-7.6 μM, 11 days) hydrochloride inhibits multi wild-type and mutant lymphoma cell lines proliferation with IC50s of 0.49-7.6 μM[1]. Cell Cytotoxicity Assay[1] Cell Line: Wild-type and mutant lymphoma cell lines Concentration: 0.49-7.6 μM Incubation Time: 11 days Result: Inhibited DOHH-2 cell (EZH2 wild-type; IC50=1.7 μM), Farage cell (EZH2 wild-type; IC50=99 nM), OCI-LY19 cell (EZH2 wild-type; IC50=6.2 μM), Toledo cell (EZH2 wild-type; IC50=7.6 μM), KARPAS-422 (EZH2 Y646N; IC50=1.8 nM), Pfeiffer (EZH2 A682G; IC50=0.49 nM), RL cell line (EZH2 Y646N; IC50=5.8 μM), SU-DHL-10 (EZH2 Y646F; IC50=5.8 nM), SU-DHL-6 (EZH2 Y646N; IC50=4.7 nM), WSU-DLCL2 (EZH2 Y646F; IC50=8.6 nM) proliferation.

Tazemetostat (EPZ-6438; 250-500 mg/kg; p.o.; twice daily; for 21-28 days) hydrochloride practically eliminates the fast-growing G401 tumors[1]. Animal Model: SCID mice bearing s.c. G401 xenografts[1] Dosage: 125 mg/kg, 250 mg/kg and 500 mg/kg Administration: Oral administration; twice daily; 28 days Result: Eliminated the fast-growing G401 tumors.

[1]. Knutson SK, et, al. Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferaseEZH2. Proc Natl Acad Sci U S A. 2013 May 7;110(19):7922-7.